WO2020141460A3 - Compounds comprising cleavable linker and uses thereof - Google Patents

Compounds comprising cleavable linker and uses thereof Download PDF

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Publication number
WO2020141460A3
WO2020141460A3 PCT/IB2020/000019 IB2020000019W WO2020141460A3 WO 2020141460 A3 WO2020141460 A3 WO 2020141460A3 IB 2020000019 W IB2020000019 W IB 2020000019W WO 2020141460 A3 WO2020141460 A3 WO 2020141460A3
Authority
WO
WIPO (PCT)
Prior art keywords
cleavable linker
ligand
functional group
active agent
compounds
Prior art date
Application number
PCT/IB2020/000019
Other languages
French (fr)
Other versions
WO2020141460A2 (en
Inventor
Taekyo PARK
Sung Ho WOO
Sunyoung Kim
Suho Park
Jongun CHO
Doohwan JUNG
Donghoon SEO
Jaeho Lee
Sangkwang LEE
Sanghyeon YUN
Jihyeon HA
Hyang Sook LEE
Okku PARK
Beomseok Seo
Sena Kim
Minah SEOL
Jina SONG
Original Assignee
Intocell, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Intocell, Inc. filed Critical Intocell, Inc.
Priority to EA202191855A priority Critical patent/EA202191855A1/en
Priority to CN202080007805.2A priority patent/CN113423431A/en
Priority to US17/419,435 priority patent/US20210393795A1/en
Priority to JP2021538388A priority patent/JP2022515885A/en
Priority to CN202111628316.1A priority patent/CN114306635A/en
Priority to KR1020217024209A priority patent/KR20210099658A/en
Priority to EP20735849.0A priority patent/EP3906063A4/en
Publication of WO2020141460A2 publication Critical patent/WO2020141460A2/en
Publication of WO2020141460A3 publication Critical patent/WO2020141460A3/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • A61K47/551—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds one of the codrug's components being a vitamin, e.g. niacinamide, vitamin B3, cobalamin, vitamin B12, folate, vitamin A or retinoic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6849—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a receptor, a cell surface antigen or a cell surface determinant
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6891—Pre-targeting systems involving an antibody for targeting specific cells
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies

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  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Cell Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)

Abstract

Provided are a compound including a cleavable linker, a use thereof, and an intermediate compound for preparing the same, and more particularly, the compound including a cleavable linker of the present invention may include an active agent (for example, a drug, a toxin, a ligand, a probe for detection, etc.) having a specific function or activity, a -S(=0)(=N-)- functional group which is capable of selectively releasing the active agent, and a functional group which triggers a chemical reaction, a physicochemical reaction and/or a biological reaction by external stimulation, and may further include a ligand (for example, oligopeptide, polypeptide, antibody, etc.) having binding specificity for a desired target receptor.
PCT/IB2020/000019 2019-01-03 2020-01-02 Compounds comprising cleavable linker and uses thereof WO2020141460A2 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
EA202191855A EA202191855A1 (en) 2019-01-03 2020-01-02 SPLITTABLE LINKER CONNECTIONS AND METHODS OF THEIR APPLICATION
CN202080007805.2A CN113423431A (en) 2019-01-03 2020-01-02 Compounds comprising a cleavable linker and uses thereof
US17/419,435 US20210393795A1 (en) 2019-01-03 2020-01-02 Compounds comprising cleavable linker and uses thereof
JP2021538388A JP2022515885A (en) 2019-01-03 2020-01-02 Compounds containing cleavable linkers and their use
CN202111628316.1A CN114306635A (en) 2019-01-03 2020-01-02 Compounds comprising a cleavable linker and uses thereof
KR1020217024209A KR20210099658A (en) 2019-01-03 2020-01-02 Compounds comprising cleavable linkers and uses thereof
EP20735849.0A EP3906063A4 (en) 2019-01-03 2020-01-02 Compounds comprising cleavable linker and uses thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962788039P 2019-01-03 2019-01-03
US62/788,039 2019-01-03

Publications (2)

Publication Number Publication Date
WO2020141460A2 WO2020141460A2 (en) 2020-07-09
WO2020141460A3 true WO2020141460A3 (en) 2020-08-27

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PCT/IB2020/000019 WO2020141460A2 (en) 2019-01-03 2020-01-02 Compounds comprising cleavable linker and uses thereof

Country Status (7)

Country Link
US (1) US20210393795A1 (en)
EP (1) EP3906063A4 (en)
JP (1) JP2022515885A (en)
KR (1) KR20210099658A (en)
CN (2) CN114306635A (en)
EA (1) EA202191855A1 (en)
WO (1) WO2020141460A2 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7174757B2 (en) 2017-07-04 2022-11-17 イントゥーセル，インコーポレーティッド Compounds containing cleavable linkers and uses thereof
US11434291B2 (en) 2019-05-14 2022-09-06 Provention Bio, Inc. Methods and compositions for preventing type 1 diabetes
US12006366B2 (en) 2020-06-11 2024-06-11 Provention Bio, Inc. Methods and compositions for preventing type 1 diabetes
CN114874287B (en) * 2022-05-20 2024-04-02 联宁（苏州）生物制药有限公司 Synthesis method of antibody coupling drug-linker LND1042

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US5279920A (en) * 1991-11-01 1994-01-18 Konica Corporation Silver halide photographic light sensitive material
JP2005291974A (en) * 2004-03-31 2005-10-20 Kyocera Chemical Corp Magnetic organic particle having feldazyl group, particle fixing method and microarray
WO2019008441A1 (en) * 2017-07-04 2019-01-10 Intocell, Inc. Compounds comprising cleavable linker and uses thereof

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JP2017503803A (en) * 2014-01-10 2017-02-02 シャンハイ バーディー バイオテック インコーポレイテッド Compounds and compositions for treating EGFR expressing tumors
KR101628872B1 (en) * 2014-05-28 2016-06-09 주식회사 레고켐 바이오사이언스 Compounds comprising self-immolative group
WO2018124758A2 (en) * 2016-12-28 2018-07-05 주식회사 인투셀 Compound bearing beta-galactoside-introduced self-immolative linker

Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
US5279920A (en) * 1991-11-01 1994-01-18 Konica Corporation Silver halide photographic light sensitive material
JP2005291974A (en) * 2004-03-31 2005-10-20 Kyocera Chemical Corp Magnetic organic particle having feldazyl group, particle fixing method and microarray
WO2019008441A1 (en) * 2017-07-04 2019-01-10 Intocell, Inc. Compounds comprising cleavable linker and uses thereof

Non-Patent Citations (3)

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Title
ADEL M. ELSOHLY, CHAWITA NETIROJJANAKUL, IOANA L. AANEI, ASTRAEA JAGER, SEAN C. BENDALL, MICHELLE E. FARKAS, GARRY P. NOLAN, MATTH: "Synthetically Modified Viral Capsids as Versatile Carriers for Use in Antibody-Based Cell Targeting", BIOCONJUGATE CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 26, no. 8, 19 August 2015 (2015-08-19), pages 1590 - 1596, XP055728784, ISSN: 1043-1802, DOI: 10.1021/acs.bioconjchem.5b00226 *
ALEXANDRA GOUASMAT, AURÉLIE LEMÉTAIS, JULIEN SOLLES, YANN BOURDREUX, JEAN-MARIE BEAU: "Catalytic Iron(III) Chloride Mediated Site-Selective Protection of Mono- and Disaccharides and One Trisaccharide", EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, WILEY-VCH, DE, vol. 2017, no. 23, 23 June 2017 (2017-06-23), DE, pages 3355 - 3361, XP055570279, ISSN: 1434-193X, DOI: 10.1002/ejoc.201700538 *
Chemical Abstract Compound, STN express. RN 88-75-5 (16 November 1984) the formula *

Also Published As

Publication number Publication date
US20210393795A1 (en) 2021-12-23
WO2020141460A2 (en) 2020-07-09
EP3906063A4 (en) 2023-03-01
CN113423431A (en) 2021-09-21
CN114306635A (en) 2022-04-12
KR20210099658A (en) 2021-08-12
JP2022515885A (en) 2022-02-22
EA202191855A1 (en) 2021-11-19
EP3906063A2 (en) 2021-11-10

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